| 产品描述： | KB-0742 Dihydrochloride 是一种有效的、选择性的、口服生物可利用的转录延长辅因子 CDK9 的小分子抑制剂，在 10 μM ATP 下抑制 CDK9/cyclin T1 的 IC50 为 6 nM |
| 靶点： |
CDK9/cyclin T1:6 nM;CDK |
| 体外研究： |
KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs in 22Rv1 cells. |
| 体内研究： |
KB-0742 is a remarkably selective CDK9 inhibitor that leads to global downregulation of nascent transcription and AR-driven prostate cancer gene expression programs and displays in vivo efficacy in CRPC- and AML-derived xenograft models. |
| 细胞实验： |
Cell lines: 22Rv1 cells Concentrations: 0–40 μM Incubation Time: 8 h Method: 22Rv1 cells are plated in 96-well plates, adding 100 μL of a 75,000 cells/mL cell suspension in RPMI media (7,500 cells per well). After 24 h, cell culture media for 22Rv1 cells is removed and replaced with media containing 5 μM of IncuCyte® Caspase-3/7 Green Apoptosis Assay Reagent and either DMSO or KB-0742 dissolved in DMSO at the appropriate final concentration. Plates are then imaged over a period of 72 h. |
| 动物实验： |
Animal Models: Male mus musculus (CB17-SCID,6-8 weeks, 18-22 g) inoculated with 22Rv1 tumor cells Dosages: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: p.o. |
| 参考文献： |
1. André Richters, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol . 2021 Feb 18;28(2):134-147.e14. |
| 溶解性： |
Soluble in DMSO、Ethanol、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.775 ml |
13.876 ml |
27.753 ml |
| 5 mM |
0.555 ml |
2.775 ml |
5.551 ml |
| 10 mM |
0.278 ml |
1.388 ml |
2.775 ml |
| 50 mM |
0.056 ml |
0.278 ml |
0.555 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
